Dual system for the central nervous system targeting and blood-brain barrier transport of a selective prolyl oligopeptidase inhibitor

Meritxell Teixidó, Esther Zurita, Laura Mendieta, Benjamí Oller-Salvia, Roger Prades, Teresa Tarragó, Ernest Giralt

Producció científica: Article en revista indexadaArticleAvaluat per experts

9 Cites (Scopus)

Resum

Less than 2% of all potential neurotherapeutics cross the blood-brain barrier (BBB). Here, we sought to build a construct with the capacity to cross this barrier, to behave as a chemical delivery system, and, once inside the central nervous system, to be transformed and then act as an enzyme inhibitor. With all this in mind, here, we describe the entire process to obtain such a compound, from the initial candidate selection to preparation of the compound library and posterior evaluation and final selection of the most promising candidates in terms of selectivity, serum stability, and BBB-transport.

Idioma originalAnglès
Pàgines (de-a)662-674
Nombre de pàgines13
RevistaBiopolymers
Volum100
Número6
DOIs
Estat de la publicacióPublicada - de nov. 2013
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